CA2831582C - (aralkylamino et heteroarylalkylamino alpha-substitues)pyrimidinyl- et 1,3,5-triazinylbenzimidazoles, compositions pharmaceutiques associees etleur utilisation dans le traitement de maladies proliferatives - Google Patents

(aralkylamino et heteroarylalkylamino alpha-substitues)pyrimidinyl- et 1,3,5-triazinylbenzimidazoles, compositions pharmaceutiques associees etleur utilisation dans le traitement de maladies proliferatives Download PDF

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CA2831582C
CA2831582C CA2831582A CA2831582A CA2831582C CA 2831582 C CA2831582 C CA 2831582C CA 2831582 A CA2831582 A CA 2831582A CA 2831582 A CA2831582 A CA 2831582A CA 2831582 C CA2831582 C CA 2831582C
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compound
optionally substituted
substituents
hydrogen
alkyl
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CA2831582A1 (fr
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S. David Brown
David J. Matthews
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Mei Pharma Inc
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Mei Pharma Inc
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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Abstract

La présente invention concerne des (aralkylamino et hétéroarylalkylamino alpha-substitués)pyrimidinyl- et 1,3,5-triazinylbenzimidazoles, par exemple, un composé de formule I, et leurs compositions pharmaceutiques, préparation et utilisation en tant qu'agents ou médicaments pour traiter des maladies prolifératives.
CA2831582A 2011-03-28 2012-03-27 (aralkylamino et heteroarylalkylamino alpha-substitues)pyrimidinyl- et 1,3,5-triazinylbenzimidazoles, compositions pharmaceutiques associees etleur utilisation dans le traitement de maladies proliferatives Active CA2831582C (fr)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201161468502P 2011-03-28 2011-03-28
US61/468,502 2011-03-28
US201161530859P 2011-09-02 2011-09-02
US61/530,859 2011-09-02
US201161560699P 2011-11-16 2011-11-16
US61/560,699 2011-11-16
PCT/US2012/030640 WO2012135160A1 (fr) 2011-03-28 2012-03-27 (aralkylamino et hétéroarylalkylamino alpha-substitués)pyrimidinyl- et 1,3,5-triazinylbenzimidazoles, compositions pharmaceutiques contenant ceux-ci et ces composés pour utilisation dans le traitement de maladies prolifératives

Publications (2)

Publication Number Publication Date
CA2831582A1 CA2831582A1 (fr) 2012-10-04
CA2831582C true CA2831582C (fr) 2019-01-08

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CA2831582A Active CA2831582C (fr) 2011-03-28 2012-03-27 (aralkylamino et heteroarylalkylamino alpha-substitues)pyrimidinyl- et 1,3,5-triazinylbenzimidazoles, compositions pharmaceutiques associees etleur utilisation dans le traitement de maladies proliferatives

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US (6) US9056852B2 (fr)
EP (1) EP2691384B1 (fr)
JP (1) JP6042406B2 (fr)
KR (1) KR101940831B1 (fr)
CN (2) CN107501241B (fr)
AU (2) AU2012236834B2 (fr)
BR (1) BR112013024907A2 (fr)
CA (1) CA2831582C (fr)
DK (1) DK2691384T3 (fr)
ES (1) ES2608967T3 (fr)
IL (1) IL228600B (fr)
MX (1) MX345238B (fr)
RU (1) RU2608742C2 (fr)
SG (1) SG193982A1 (fr)
TW (1) TWI572599B (fr)
WO (1) WO2012135160A1 (fr)
ZA (1) ZA201307224B (fr)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2831582C (fr) 2011-03-28 2019-01-08 Mei Pharma, Inc. (aralkylamino et heteroarylalkylamino alpha-substitues)pyrimidinyl- et 1,3,5-triazinylbenzimidazoles, compositions pharmaceutiques associees etleur utilisation dans le traitement de maladies proliferatives
WO2012135175A1 (fr) * 2011-03-28 2012-10-04 Pathway Therapeutics Inc. (cycloalkylamino ou hétérocyclylamino alpha-substitué) pyrimidinyl et 1,3,5-triazinyl benzimidazoles, compositions pharmaceutiques les contenant et leur utilisation dans le traitement des maladies prolifératives
KR20210010958A (ko) 2012-11-08 2021-01-28 리젠 파마슈티컬스 소시에떼 아노님 Pde4 억제제 및 pi3 델타 또는 이중 pi3 델타-감마 키나아제 억제제를 함유하는 약제학적 조성물
CN105102448B (zh) 2013-02-28 2018-03-06 百时美施贵宝公司 作为rock1和rock2抑制剂的苯基吡唑衍生物
AR094929A1 (es) 2013-02-28 2015-09-09 Bristol Myers Squibb Co Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2
JP6441910B2 (ja) 2013-09-30 2018-12-19 シャンハイ インリ ファーマシューティカル カンパニー リミティド 縮合ピリミジン化合物、中間体、その調製方法、組成物及び使用
EP3059238B1 (fr) 2013-10-16 2020-05-27 Shanghai Yingli Pharmaceutical Co. Ltd. Composé hétérocyclique condensé, son procédé de préparation, composition pharmaceutique et leurs utilisations
CN103992228A (zh) * 2014-05-26 2014-08-20 南京工业大学 一种盐酸芬特明的合成方法
KR20190058550A (ko) 2016-09-19 2019-05-29 메이 파마, 아이엔씨. 병용 요법
MX2019013862A (es) * 2017-05-23 2020-01-20 Mei Pharma Inc Terapia de combinacion.
WO2019036489A1 (fr) * 2017-08-14 2019-02-21 Mei Pharma, Inc. Polythérapie
JP2021517116A (ja) * 2018-03-21 2021-07-15 エムイーアイ ファーマ，インク． 併用療法
CN112189012B (zh) 2018-04-10 2024-02-13 神经孔疗法股份有限公司 作为pi3激酶和自噬途径的调节剂的三取代芳基和杂芳基衍生物
SG11202008851UA (en) * 2018-04-10 2020-10-29 Neuropore Therapies Inc Morpholine derivates as inhibitors of vps34
MA53236A (fr) * 2018-08-14 2021-06-23 Mei Pharma Inc Traitement des malignités des lymphocytes b
MX2021001765A (es) * 2018-08-14 2021-04-19 Mei Pharma Inc Tratamiento del linfoma follicular reicindido.
CN112839651A (zh) * 2018-08-14 2021-05-25 梅制药公司 联合疗法
AU2019382737A1 (en) * 2018-11-20 2021-05-20 Bayer Aktiengesellschaft α2-adrenoceptor subtype C (alpha-2C) antagonists for the treatment of sleep apnea
TW202038945A (zh) * 2018-12-21 2020-11-01 美商梅製藥公司 組合療法
MX2022012339A (es) * 2020-04-07 2022-10-27 Mei Pharma Inc Preparacion de un 1,3,5-triazinil benzimidazol.
WO2022197884A1 (fr) 2021-03-18 2022-09-22 Teva Pharmaceuticals International Gmbh Formes à l'état solide de zandélisib et leurs sels

Family Cites Families (169)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3536809A (en) 1969-02-17 1970-10-27 Alza Corp Medication method
US3598123A (en) 1969-04-01 1971-08-10 Alza Corp Bandage for administering drugs
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US3916899A (en) 1973-04-25 1975-11-04 Alza Corp Osmotic dispensing device with maximum and minimum sizes for the passageway
US4008719A (en) 1976-02-02 1977-02-22 Alza Corporation Osmotic system having laminar arrangement for programming delivery of active agent
US4410545A (en) 1981-02-13 1983-10-18 Syntex (U.S.A.) Inc. Carbonate diester solutions of PGE-type compounds
US4328245A (en) 1981-02-13 1982-05-04 Syntex (U.S.A.) Inc. Carbonate diester solutions of PGE-type compounds
US4409239A (en) 1982-01-21 1983-10-11 Syntex (U.S.A.) Inc. Propylene glycol diester solutions of PGE-type compounds
HU196714B (en) 1984-10-04 1989-01-30 Monsanto Co Process for producing non-aqueous composition comprising somatotropin
IE58110B1 (en) 1984-10-30 1993-07-14 Elan Corp Plc Controlled release powder and process for its preparation
US5052558A (en) 1987-12-23 1991-10-01 Entravision, Inc. Packaged pharmaceutical product
US5033252A (en) 1987-12-23 1991-07-23 Entravision, Inc. Method of packaging and sterilizing a pharmaceutical product
US5073543A (en) 1988-07-21 1991-12-17 G. D. Searle & Co. Controlled release formulations of trophic factors in ganglioside-lipsome vehicle
US5612059A (en) 1988-08-30 1997-03-18 Pfizer Inc. Use of asymmetric membranes in delivery devices
IT1229203B (it) 1989-03-22 1991-07-25 Bioresearch Spa Impiego di acido 5 metiltetraidrofolico, di acido 5 formiltetraidrofolico e dei loro sali farmaceuticamente accettabili per la preparazione di composizioni farmaceutiche in forma a rilascio controllato attive nella terapia dei disturbi mentali organici e composizioni farmaceutiche relative.
PH30995A (en) 1989-07-07 1997-12-23 Novartis Inc Sustained release formulations of water soluble peptides.
US5120548A (en) 1989-11-07 1992-06-09 Merck & Co., Inc. Swelling modulated polymeric drug delivery device
US5585112A (en) 1989-12-22 1996-12-17 Imarx Pharmaceutical Corp. Method of preparing gas and gaseous precursor-filled microspheres
IT1246382B (it) 1990-04-17 1994-11-18 Eurand Int Metodo per la cessione mirata e controllata di farmaci nell'intestino e particolarmente nel colon
US5733566A (en) 1990-05-15 1998-03-31 Alkermes Controlled Therapeutics Inc. Ii Controlled release of antiparasitic agents in animals
US5543390A (en) 1990-11-01 1996-08-06 State Of Oregon, Acting By And Through The Oregon State Board Of Higher Education, Acting For And On Behalf Of The Oregon Health Sciences University Covalent microparticle-drug conjugates for biological targeting
US5580578A (en) 1992-01-27 1996-12-03 Euro-Celtique, S.A. Controlled release formulations coated with aqueous dispersions of acrylic polymers
US5323907A (en) 1992-06-23 1994-06-28 Multi-Comp, Inc. Child resistant package assembly for dispensing pharmaceutical medications
TW333456B (en) 1992-12-07 1998-06-11 Takeda Pharm Ind Co Ltd A pharmaceutical composition of sustained-release preparation the invention relates to a pharmaceutical composition of sustained-release preparation which comprises a physiologically active peptide.
US5591767A (en) 1993-01-25 1997-01-07 Pharmetrix Corporation Liquid reservoir transdermal patch for the administration of ketorolac
US6274552B1 (en) 1993-03-18 2001-08-14 Cytimmune Sciences, Inc. Composition and method for delivery of biologically-active factors
US5523092A (en) 1993-04-14 1996-06-04 Emory University Device for local drug delivery and methods for using the same
US5985307A (en) 1993-04-14 1999-11-16 Emory University Device and method for non-occlusive localized drug delivery
US6087324A (en) 1993-06-24 2000-07-11 Takeda Chemical Industries, Ltd. Sustained-release preparation
US6004534A (en) 1993-07-23 1999-12-21 Massachusetts Institute Of Technology Targeted polymerized liposomes for improved drug delivery
IT1270594B (it) 1994-07-07 1997-05-07 Recordati Chem Pharm Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida
US5759542A (en) 1994-08-05 1998-06-02 New England Deaconess Hospital Corporation Compositions and methods for the delivery of drugs by platelets for the treatment of cardiovascular and other diseases
EP0711804A3 (fr) 1994-11-14 1999-09-22 Ciba SC Holding AG Stabilisateurs à la lumière latents
US5660854A (en) 1994-11-28 1997-08-26 Haynes; Duncan H Drug releasing surgical implant or dressing material
US6316652B1 (en) 1995-06-06 2001-11-13 Kosta Steliou Drug mitochondrial targeting agents
US5798119A (en) 1995-06-13 1998-08-25 S. C. Johnson & Son, Inc. Osmotic-delivery devices having vapor-permeable coatings
WO1997001331A2 (fr) 1995-06-27 1997-01-16 Takeda Chemical Industries, Ltd. Production de preparations a liberation prolongee
JP3512911B2 (ja) 1995-07-11 2004-03-31 富士写真フイルム株式会社 紫外線吸収剤前駆体化合物、それを含有する感光性樹脂組成物及び画像形成方法
TW448055B (en) 1995-09-04 2001-08-01 Takeda Chemical Industries Ltd Method of production of sustained-release preparation
JP2909418B2 (ja) 1995-09-18 1999-06-23 株式会社資生堂 薬物の遅延放出型マイクロスフイア
US6039975A (en) 1995-10-17 2000-03-21 Hoffman-La Roche Inc. Colon targeted delivery system
US5980945A (en) 1996-01-16 1999-11-09 Societe De Conseils De Recherches Et D'applications Scientifique S.A. Sustained release drug formulations
TW345603B (en) 1996-05-29 1998-11-21 Gmundner Fertigteile Gmbh A noise control device for tracks
US6264970B1 (en) 1996-06-26 2001-07-24 Takeda Chemical Industries, Ltd. Sustained-release preparation
US6419961B1 (en) 1996-08-29 2002-07-16 Takeda Chemical Industries, Ltd. Sustained release microcapsules of a bioactive substance and a biodegradable polymer
IL129242A0 (en) 1996-10-01 2000-02-17 Cima Labs Inc Taste-masked microcapsule compositions and methods of manufacture
CA2217134A1 (fr) 1996-10-09 1998-04-09 Sumitomo Pharmaceuticals Co., Ltd. Formulation a liberation-retard
DK0839525T3 (da) 1996-10-31 2004-11-29 Takeda Pharmaceutical Præparat med forlænget frigivelse
US6131570A (en) 1998-06-30 2000-10-17 Aradigm Corporation Temperature controlling device for aerosol drug delivery
DK0946169T3 (da) 1996-12-20 2003-04-22 Takeda Chemical Industries Ltd Fremgangsmåde til fremstilling af et præparat med vedvarende frigivelse
US5891474A (en) 1997-01-29 1999-04-06 Poli Industria Chimica, S.P.A. Time-specific controlled release dosage formulations and method of preparing same
US6120751A (en) 1997-03-21 2000-09-19 Imarx Pharmaceutical Corp. Charged lipids and uses for the same
US6060082A (en) 1997-04-18 2000-05-09 Massachusetts Institute Of Technology Polymerized liposomes targeted to M cells and useful for oral or mucosal drug delivery
CA2297326C (fr) 1997-07-24 2007-03-20 Zenyaku Kogyo Kabushiki Kaisha Composes heterocycliques et agent antitumoral contenant lesdits composes utilises comme ingredients actifs
JPH11174638A (ja) 1997-12-08 1999-07-02 Konica Corp ハロゲン化銀カラー写真感光材料
US6350458B1 (en) 1998-02-10 2002-02-26 Generex Pharmaceuticals Incorporated Mixed micellar drug deliver system and method of preparation
US6613358B2 (en) 1998-03-18 2003-09-02 Theodore W. Randolph Sustained-release composition including amorphous polymer
US6048736A (en) 1998-04-29 2000-04-11 Kosak; Kenneth M. Cyclodextrin polymers for carrying and releasing drugs
KR19990085365A (ko) 1998-05-16 1999-12-06 허영섭 지속적으로 약물 조절방출이 가능한 생분해성 고분자 미립구 및그 제조방법
US6248363B1 (en) 1999-11-23 2001-06-19 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
US6271359B1 (en) 1999-04-14 2001-08-07 Musc Foundation For Research Development Tissue-specific and pathogen-specific toxic agents and ribozymes
CA2383546A1 (fr) * 1999-06-30 2001-01-04 William H. Parsons Composes inhibiteurs de la src kinase
JP4794793B2 (ja) * 1999-12-28 2011-10-19 ファーマコペイア， インコーポレイテッド Ｎ−ヘテロ環ＴＮＦ−α発現阻害剤
NZ522076A (en) 2000-04-25 2005-08-26 Icos Corp Inhibitors of human phosphatidyl-inositol 3-kinase delta
AU6513701A (en) 2000-05-30 2001-12-11 Advanced Res & Tech Inst Compositions and methods for identifying agents which modulate pten function andpi-3 kinase pathways
AP2001002264A0 (en) 2000-08-30 2001-09-30 Pfizer Prod Inc Sustained release formulations for growth hormone secretagogues.
US7071189B2 (en) 2001-04-27 2006-07-04 Zenyaku Kogyo Kabushiki Kaisha Heterocyclic compound and antitumor agent containing the same as active ingredient
DE10207037A1 (de) 2002-02-20 2003-08-28 Bayer Cropscience Gmbh 2-Amino-4-bicyclyamino-6H-1,3.5-triazine, Verfahren zu deren Herstellung und deren Verwendung als Herbizide und Pflanzenwachstumsregulatoren
DE60314603T2 (de) 2002-03-15 2008-02-28 Vertex Pharmaceuticals Inc., Cambridge Zusammensetzungen brauchbar als protein-kinase-inhibitoren
US7179826B2 (en) 2002-03-15 2007-02-20 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
ATE466580T1 (de) 2002-03-15 2010-05-15 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
DE60332604D1 (de) 2002-03-15 2010-07-01 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
WO2003097862A1 (fr) 2002-05-17 2003-11-27 Kyowa Hakko Kogyo Co., Ltd. Procede de recherche de matiere possedant une activite antidiabetique
KR101046015B1 (ko) 2002-10-25 2011-07-01 젠야쿠코교가부시키가이샤 헤테로고리 화합물 및 이것을 유효성분으로 하는 항종양제
ES2412273T3 (es) * 2002-11-21 2013-07-10 Novartis Ag Inhibidores de 2-morfolín-4-pirimidinas como inhibidores de fosfotidilinositol (PI) 3-quinasa y su uso en el tratamiento del cáncer.
WO2005028467A1 (fr) 2003-09-15 2005-03-31 Anadys Pharmaceuticals, Inc. Composes heteroaromatiques et aromatiques a substitution 3,5-diaminopiperidine antibacteriens
PT1704145E (pt) 2004-01-12 2012-09-04 Ym Biosciences Australia Pty Inibidores de quinase seletivos
JP4733021B2 (ja) 2004-03-31 2011-07-27 全薬工業株式会社 複素環式化合物及びそれを有効成分とする抗悪性腫瘍剤
RS51601B (en) 2004-08-26 2011-08-31 Pfizer Inc. PYRAZOLS SUBSTITUTED BY AMINOHETEROARYL UNITS AS PROTEIN KINASE INHIBITORS
WO2006053227A2 (fr) 2004-11-10 2006-05-18 Synta Pharmaceuticals Corp. Composes modulateurs de la il-12
TW200628463A (en) 2004-11-10 2006-08-16 Synta Pharmaceuticals Corp Heteroaryl compounds
KR101296884B1 (ko) 2005-03-11 2013-08-14 젠야쿠코교가부시키가이샤 활성 성분으로서 헤테로시클릭 화합물을 포함하는 면역억제제 및 항암제
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
GB0525081D0 (en) 2005-12-09 2006-01-18 Astrazeneca Ab Pyrimidine derivatives
GB0525080D0 (en) 2005-12-09 2006-01-18 Astrazeneca Ab Pyrimidine derivatives
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
US20070244110A1 (en) 2006-04-14 2007-10-18 Zenyaku Kogyo Kabushiki Kaisha Treatment of prostate cancer, melanoma or hepatic cancer
KR101402474B1 (ko) 2006-04-26 2014-06-19 제넨테크, 인크. 포스포이노시티드 3-키나제 억제제 화합물 및 이를 포함하는 약학적 조성물
TWI498332B (zh) 2006-04-26 2015-09-01 Hoffmann La Roche 作為pi3k抑制劑之嘧啶衍生物及相關製備方法、醫藥組合物、用途、套組及產物
ES2657635T3 (es) 2006-08-08 2018-03-06 Chugai Seiyaku Kabushiki Kaisha Derivado de pirimidina como inhibidor de PI3K y uso del mismo
WO2008032060A1 (fr) 2006-09-14 2008-03-20 Astrazeneca Ab Dérivés de 4-benzimidaz0lyl-6-m0rph0lin0-2-pipérazinylpyrimidine utilisés comme inhibiteurs de p13k et mtor dans le traitement de troubles prolifératifs
WO2008032077A1 (fr) 2006-09-14 2008-03-20 Astrazeneca Ab Dérivés de pyrimidine
US20100022534A1 (en) 2006-09-14 2010-01-28 Astrazeneca 2-benzimidazolyl-6-morpholino-4- (azetidine, pyrrolidine, piperidine or azepine) pyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032041A1 (fr) 2006-09-14 2008-03-20 Astrazeneca Ab Dérivés de la pyrimidine à activité inhibitrice contre les enzymes pi3k
WO2008032027A1 (fr) 2006-09-14 2008-03-20 Astrazeneca Ab Dérivés de pyrimidine
JP2010503650A (ja) 2006-09-14 2010-02-04 アストラゼネカ アクチボラグ 増殖性疾患の治療のための、ｐｉ３ｋおよびｍｔｏｒ阻害剤としての２−ベンズイミダゾリル−６−モルホリノ−４−ピペリジン−４−イルピリミジン誘導体
JP2010503651A (ja) 2006-09-14 2010-02-04 アストラゼネカ アクチボラグ 増殖性障害の治療用のＰＩ３Ｋ及びｍＴＯＲ阻害剤としての２−ベンゾイミダゾリル−６−モルホリノ−フェニルピリミジン誘導体
WO2008032033A1 (fr) 2006-09-14 2008-03-20 Astrazeneca Ab Dérivés de 4-benzimidazolyl-2-morpholino-6-pipérazinylpyrimidine utilisés en tant que pi3k et inhibiteurs de mtor destinés au traitement de troubles prolifératifs
WO2008032036A1 (fr) 2006-09-14 2008-03-20 Astrazeneca Ab Dérivés de 6-benzimidazolyl-2-morpholino-4-(azétidine, pyrrolidine, piperidine ou azépine) pyrimidine comme inhibiteurs de pi3k et mtor pour le traitement de troubles prolifératifs
WO2008032091A1 (fr) 2006-09-14 2008-03-20 Astrazeneca Ab Dérivés de pyrimidine
EP2057147A1 (fr) 2006-09-14 2009-05-13 Astra Zeneca AB Dérivés de pyrimidine
WO2008032089A1 (fr) 2006-09-14 2008-03-20 Astrazeneca Ab Dérivés de 4-benzimidaz0lyl-2-m0rph0lin0-6-piperidin-4-ylpyrimidine utilisés comme inhibiteurs de p13k et de mtor pour le traitement de troubles prolifératifs
KR20090108124A (ko) 2007-02-06 2009-10-14 노파르티스 아게 Ｐｉ 3-키나제 억제제 및 그의 사용 방법
US20080221103A1 (en) 2007-03-09 2008-09-11 Orchid Research Laboratories Ltd. New heterocyclic compounds
US20080233127A1 (en) 2007-03-21 2008-09-25 Wyeth Imidazolopyrimidine analogs and their use as pi3 kinase and mtor inhibitors
US20080234262A1 (en) 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
CN101730699A (zh) * 2007-03-21 2010-06-09 百时美施贵宝公司 可用于治疗增殖性、变应性、自身免疫性和炎症性疾病的稠合杂环化合物
JP2010529193A (ja) 2007-06-11 2010-08-26 ミイカナ セラピューティクス インコーポレイテッド 置換ピラゾール化合物
CN101801963A (zh) 2007-07-09 2010-08-11 阿斯利康(瑞典)有限公司 用于治疗增殖性疾病的三取代的嘧啶衍生物
WO2009045174A1 (fr) 2007-10-05 2009-04-09 S*Bio Pte Ltd 2 -morpholinylpurines en tant qu'inhibiteurs de pi3k
MY150993A (en) 2007-10-05 2014-03-31 Verastem Inc Pyrimidine substituted purine derivatives
CA2706536C (fr) 2007-11-22 2016-04-19 Tadaaki Sugama Forme amorphe de compose heterocyclique, dispersion solide et preparation pharmaceutique comprenant chacune ladite forme amorphe et procede de production de ladite forme amorphe
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
KR20100113567A (ko) 2008-01-15 2010-10-21 와이어쓰 엘엘씨 3Ｈ-[1,2,3]트라이아졸로[4,5-Ｄ]피리미딘 화합물, ｍＴＯＲ 카이네이즈 및 ＰＩ3 카이네이즈 억제제로서의 이의 용도 및 합성
WO2009093981A1 (fr) 2008-01-23 2009-07-30 S Bio Pte Ltd Composés de triazine comme inhibiteurs de la kinase
US20090192176A1 (en) 2008-01-30 2009-07-30 Wyeth 1H-PYRAZOLO[3,4-D]PYRIMIDINE, PURINE, 7H-PURIN-8(9H)-ONE, 3H-[1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE, AND THIENO[3,2-D]PYRIMIDINE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES
CL2009000241A1 (es) 2008-02-07 2010-09-03 Chugai Pharmaceutical Co Ltd Compuestos derivados de 5-(2-morfolin-4-il-7h-pirrolo[2,3-d]pirimidin-4-il)pirimidin-2-ilamina; proceso de preparacion; composicion farmaceutica; y uso de los compuestos para tratar o prevenir una enfermedad proliferativa tal como el cancer.
EP2276750A2 (fr) 2008-03-27 2011-01-26 Auckland Uniservices Limited Pyrimidines et triazines substituées, et leur utilisation en thérapie anticancéreuse
UA99361C2 (uk) 2008-05-23 2012-08-10 Уайт Елелсі ТРИАЗИНИ ЯК ІНГІБІТОРИ PІ3-КІНАЗИ І mTOR
US20110105500A1 (en) 2008-06-27 2011-05-05 S*Bio Pte Ltd. Pyrazine substituted purines
CN102089308A (zh) 2008-07-07 2011-06-08 艾科睿控股公司 Pi3k亚型选择性抑制剂
WO2010048149A2 (fr) 2008-10-20 2010-04-29 Kalypsys, Inc. Modulateurs hétérocycliques de gpr119 pour le traitement d'une maladie
GB2465405A (en) 2008-11-10 2010-05-19 Univ Basel Triazine, pyrimidine and pyridine analogues and their use in therapy
JP5794919B2 (ja) 2008-11-13 2015-10-14 ギリアード カリストガ エルエルシー 血液学的な悪性疾患のための療法
MX2011008444A (es) * 2009-02-12 2011-09-06 Astellas Pharma Inc Derivado de heteroanillo.
WO2010110686A1 (fr) 2009-03-27 2010-09-30 Pathway Therapeutics Limited Pyrimidinyl et 1,3,5-triazinyl benzimidazoles et leur utilisation en thérapie anticancéreuse
RU2011143359A (ru) 2009-03-27 2013-05-10 Патвэй Терапьютикс, Инк. Примидинил- и 1,3,5-триазинилбензимидазолсульфонамиды и их применение в терапии рака
SG182247A1 (en) 2009-05-27 2012-08-30 Hoffmann La Roche Bicyclic indole-pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use
AU2010254161A1 (en) 2009-05-27 2011-11-10 F. Hoffmann-La Roche Ag Bicyclic pyrimidine PI3K inhibitor compounds selective for p110 delta, and methods of use
CA2765823A1 (fr) 2009-06-25 2010-12-29 Amgen Inc. Composes heterocycliques et leurs utilisations
WO2010151735A2 (fr) 2009-06-25 2010-12-29 Amgen Inc. Composés hétérocycliques et leurs utilisations
MX2011013667A (es) 2009-06-25 2012-03-06 Amgen Inc Compuestos heterociclicos y sus usos.
AU2010265974B2 (en) 2009-06-25 2014-09-11 Amgen Inc. Polycyclic derivatives of pyridine and their use in the treatment of (inter alia) rheumatoid arthritis and similar diseases
EP3072890B1 (fr) * 2009-07-07 2018-10-17 MEI Pharma, Inc. Pyrimidinyl et 1,3,5-triazinyl benzimidazoles et leur utilisation dans la thérapie du cancer
EA023931B1 (ru) * 2010-08-10 2016-07-29 Астеллас Фарма Инк. Гетероциклическое соединение
AU2011338530B2 (en) 2010-12-06 2017-06-15 Follica, Inc. Methods for treating baldness and promoting hair growth
WO2012129562A2 (fr) 2011-03-24 2012-09-27 The Scripps Research Institute Composés et procédés pour l'induction de la chondrogenèse
WO2012135166A1 (fr) 2011-03-28 2012-10-04 Pathway Therapeutics Inc. (arylamino et hétérocyclylamino à cycle condensé)pyrimidinyl- et 1,3,5-triazinylbenzimidazoles, compositions pharmaceutiques de ceux-ci et leur utilisation dans le traitement de maladies prolifératives
WO2012135175A1 (fr) 2011-03-28 2012-10-04 Pathway Therapeutics Inc. (cycloalkylamino ou hétérocyclylamino alpha-substitué) pyrimidinyl et 1,3,5-triazinyl benzimidazoles, compositions pharmaceutiques les contenant et leur utilisation dans le traitement des maladies prolifératives
CA2831582C (fr) 2011-03-28 2019-01-08 Mei Pharma, Inc. (aralkylamino et heteroarylalkylamino alpha-substitues)pyrimidinyl- et 1,3,5-triazinylbenzimidazoles, compositions pharmaceutiques associees etleur utilisation dans le traitement de maladies proliferatives
EP2723745A1 (fr) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Composés utiles comme inhibiteurs de la kinase atr
JP2014522818A (ja) 2011-06-22 2014-09-08 バーテックス ファーマシューティカルズ インコーポレイテッド Ａｔｒキナーゼ阻害剤として有用な化合物
EP2723746A1 (fr) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Composés inhibiteurs de la kinase atr
WO2013006408A1 (fr) 2011-07-01 2013-01-10 Tempero Pharmaceuticals, Inc. Composés et procédés
JP6100274B2 (ja) 2011-11-11 2017-03-22 メルク パテント ゲーエムベーハー アリールアミンの調製方法
UA116544C2 (uk) 2012-08-09 2018-04-10 Селджин Корпорейшн Спосіб лікування раку з використанням 3-(4-((4-(морфолінометил)бензил)оксі)-1-оксоізоіндолін-2-іл)піперидин-2,6-діону
WO2014055647A1 (fr) 2012-10-03 2014-04-10 Mei Pharma, Inc. (sulfinyl et sulfonyl benzimidazolyl) pyrimidines et triazines, compositions pharmaceutiques les contenant, et leur utilisation pour traiter les maladies prolifératives
US9963452B2 (en) 2013-03-14 2018-05-08 Augusta Pharmaceuticals Inc. Methods, compounds, and compositions for inhibition of ROS
EP2832358A1 (fr) 2013-08-02 2015-02-04 Bionsil S.r.l. Kit pharmaceutique pour utilisation dans le traitement de cancer du côlon et colorectal
AU2014358868A1 (en) 2013-12-05 2016-06-09 Acerta Pharma B.V. Therapeutic combination of a PI3K inhibitor and a BTK inhibitor
EP3107901B1 (fr) 2014-02-19 2020-04-01 Piramal Enterprises Limited Composés pouvant être utilisés à titre d'agonistes de gpr120
US9949971B2 (en) 2014-06-17 2018-04-24 Acerta Pharma B.V. Therapeutic combinations of a BTK inhibitor, a PI3K inhibitor and/or a JAK-2 inhibitor
CN107072984B (zh) 2014-07-15 2021-10-01 约翰·霍普金斯大学 源自骨髓的抑制细胞的抑制和免疫检查点阻断
WO2016024227A1 (fr) 2014-08-11 2016-02-18 Acerta Pharma B.V. Inhibiteurs de btk pour le traitement de tumeurs solides par modulation du micro-environnement tumoral
WO2016024228A1 (fr) 2014-08-11 2016-02-18 Acerta Pharma B.V. Combinaisons thérapeutiques associant un inhibiteur de btk, un inhibiteur de pi3k, un inhibiteur de jak-2, un inhibiteur de pd-1 et/ou un inhibiteur de pd-l1
RS60349B8 (sr) 2014-09-23 2022-10-31 Hoffmann La Roche Postupak upotrebe anti-cd79b imunokonjugata
JP6935064B2 (ja) 2014-12-24 2021-09-15 エルジー・ケム・リミテッド Ｇｐｒ１２０アゴニストとしてのビアリール誘導体
MX2018000880A (es) 2015-07-20 2018-08-24 Genzyme Corp Inhibidores del receptor del factor estimulante de colonias 1 (csf-1r).
EP3341080A4 (fr) 2015-08-24 2019-03-20 Epizyme Inc Méthode de traitement du cancer
TW201725044A (zh) 2015-10-01 2017-07-16 基利科學股份有限公司 用於治療癌症之btk抑制劑及查核點抑制劑之組合
WO2017066705A1 (fr) 2015-10-14 2017-04-20 Aquinnah Pharmaceuticals, Inc. Composés, compositions et méthodes d'utilisation contre des granules de stress
CA3031542A1 (fr) 2016-07-20 2018-01-25 University Of Utah Research Foundation Lymphocytes car-t cd229 et leurs procedes d'utilisation
WO2018060833A1 (fr) 2016-09-27 2018-04-05 Novartis Ag Schéma posologique pour l'alpelisib, un inhibiteur de la phosphatidylinositol 3-kinase spécifique de l'isoforme alpha
MX2019013862A (es) 2017-05-23 2020-01-20 Mei Pharma Inc Terapia de combinacion.
WO2019036489A1 (fr) 2017-08-14 2019-02-21 Mei Pharma, Inc. Polythérapie
JP2021517116A (ja) 2018-03-21 2021-07-15 エムイーアイ ファーマ，インク． 併用療法
MA53236A (fr) 2018-08-14 2021-06-23 Mei Pharma Inc Traitement des malignités des lymphocytes b
MX2021001765A (es) 2018-08-14 2021-04-19 Mei Pharma Inc Tratamiento del linfoma follicular reicindido.
TW202038945A (zh) 2018-12-21 2020-11-01 美商梅製藥公司 組合療法

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AU2016201558A1 (en) 2016-03-31
KR101940831B1 (ko) 2019-01-21
AU2012236834A1 (en) 2013-05-02
MX345238B (es) 2017-01-23
ZA201307224B (en) 2014-12-23
CN103582636A (zh) 2014-02-12
JP2014509647A (ja) 2014-04-21
US12059422B2 (en) 2024-08-13
KR20140049982A (ko) 2014-04-28
US11400097B2 (en) 2022-08-02
US20120252802A1 (en) 2012-10-04
US10603324B2 (en) 2020-03-31
RU2608742C2 (ru) 2017-01-23
AU2016201558B2 (en) 2018-01-25
US20150265625A1 (en) 2015-09-24
WO2012135160A1 (fr) 2012-10-04
IL228600B (en) 2018-05-31
US20200316080A1 (en) 2020-10-08
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AU2012236834B2 (en) 2015-12-10
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US20200009151A1 (en) 2020-01-09
US20220323449A1 (en) 2022-10-13
CN107501241A (zh) 2017-12-22
TW201245181A (en) 2012-11-16
EP2691384B1 (fr) 2016-10-26
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US10064868B2 (en) 2018-09-04
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US20190083506A1 (en) 2019-03-21
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